【摘要】 以氟苯和戊二酸酐为起始原料,经傅-克反应、羰基保护、水解、酰胺化、偶联反应,合成了依折麦布(Ezetimibe)的重要中间体(S)-3-{4-[2-(4-氟苯基)-[1,3]-二氧杂环戊烷-2-基]-丁酰}-4-苯基-噁唑烷-2-酮(1),总收率36.7%,该工艺反应条件温和、原料价廉易得、收率较高,具有工业化前景。更多还原

【Abstract】 (S)-3-{4-(2-(4-FluorophenyL)-dioxolane-2-yl]-butyril)-4 phenyl-oxazolidine-2-one(1) is a key intermediate for the preparation of Ezetimibe.1 was synthesized starting from fluorobenzene and glutaric anhydride,via Friedel-crafts alkylation,carbonyl protection,hydrolysis,amidation and coupling,in overall yield of 36.7%.The results showed that this synthetic route is suitable for industrial production with advantages of low cost,mild reaction conditions,and high yield.更多还原